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AT7867

Cat. No. M1654
AT7867 Structure
Size Price Availability Quantity
5mg USD 150 In stock
10mg USD 270 In stock
50mg USD 810 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AT7867 as a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A. This ATP-competitive small molecule potently inhibits both AKT and p70S6K activity at the cellular level, as measured by inhibition of GSK3β and S6 ribosomal protein phosphorylation, and also causes growth inhibition in a range of human cancer cell lines as a single agent.

Protocol
Cell Experiment
Cell lines PTEN-negative U87MG human glioblastoma cells
Preparation method Alamar Blue Cell Proliferation Assay.
Cells were plated in 96-well microplates at 5000 cells per well in medium supplemented with 10% FBS, and grown for 24 hours before treatment with AT7867. Inhibitor or vehicle control was added to the cells for 72 hours. Following this, Alamar Blue solution (BioSource, Nivelle Belgium) was added as stated in the manufacturer's instructions. The IC50 value for each inhibitor was calculated in GraphPad Prism (San Diego, USA) using non-linear regression analysis and a sigmoidal dose-response (variable slope) equation.
Concentrations 0~100 μM
Incubation time 72 h
Animal Experiment
Animal models athymic BALB/c mice bearing MES-SA and U87MG human glioblastoma xenograft tumors
Formulation 10% DMSO, 90% saline
Dosages 20mg/kg or 90mg/kg once every 3 days
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 337.85
Formula C20H20ClN3
CAS Number 857531-00-1
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth.
Grimshaw KM, et al. Mol Cancer Ther. 2010 May;9(5):1100-10. PMID: 20423992.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AT7867 supplier, Akt, inhibitors

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